List of works - Steve Sideris

4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase

scientific article

A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors

scientific article published on 23 July 2013

A plate-based assay to measure cellular ERK substrate phosphorylation: utility for drug discovery of the MAPK-signaling cascade

scientific article

Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 3: Importance of the indole orientation

scientific article published on 4 March 2008

Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice

scientific article published on 26 August 2016

Chip-Based Analysis of Protein−Protein Interactions by Fluorescence Detection and On-Chip Immunoprecipitation Combined with μLC−MS/MS Analysis ⬇️

scientific article published on November 15, 2003

Correction to Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study

scientific article published on 11 March 2016

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.

scientific article

Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer

scientific article

Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and ro

scientific article published on 3 June 2013

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.

scientific article published on 16 February 2016

Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor

scientific article

Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation

scientific article

Discovery of the 1,7-diazacarbazole class of inhibitors of checkpoint kinase 1

scientific article

Establishment of intein-mediated protein ligation under denaturing conditions: C-terminal labeling of a single-chain antibody for biochip screening

scientific article

Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase

scientific article

Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase

scientific article

Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor

scientific article published on 12 March 2010

Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase

scientific article

Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase

scientific article

Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition

scientific article

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study

scientific article

Noncovalent wild-type-sparing inhibitors of EGFR T790M

scientific article published on 10 December 2012

Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.

scientific article published on 15 April 2011

Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.

scientific article published on 12 December 2012

Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.

scientific article published on 17 December 2015

Pyrimidine-based inhibitors of CaMKIIdelta

scientific article published on 4 March 2008

Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).

scientific article

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

scientific article

Structure of the BRAF-MEK complex reveals a kinase activity independent role for BRAF in MAPK signaling

scientific article

Structure-based design of thienobenzoxepin inhibitors of PI3-kinase ⬇️

scientific article published on May 13, 2011

Targeting ferroptosis: A novel therapeutic strategy for the treatment of mitochondrial disease-related epilepsy

article

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.

scientific article published on 11 September 2012

List of works by Steve Sideris

4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase

A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors

A plate-based assay to measure cellular ERK substrate phosphorylation: utility for drug discovery of the MAPK-signaling cascade

Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 3: Importance of the indole orientation

Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice

Chip-Based Analysis of Protein−Protein Interactions by Fluorescence Detection and On-Chip Immunoprecipitation Combined with μLC−MS/MS Analysis ⬇️

Correction to Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.

Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer

Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and ro

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.

Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor

Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation

Discovery of the 1,7-diazacarbazole class of inhibitors of checkpoint kinase 1

Establishment of intein-mediated protein ligation under denaturing conditions: C-terminal labeling of a single-chain antibody for biochip screening

Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase

Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase

Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor

Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase

Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase

Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study

Noncovalent wild-type-sparing inhibitors of EGFR T790M

Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.

Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.

Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.

Pyrimidine-based inhibitors of CaMKIIdelta

Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

Structure of the BRAF-MEK complex reveals a kinase activity independent role for BRAF in MAPK signaling

Structure-based design of thienobenzoxepin inhibitors of PI3-kinase ⬇️

Targeting ferroptosis: A novel therapeutic strategy for the treatment of mitochondrial disease-related epilepsy

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.